Page last updated: 2024-12-06
flosulide
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 71246 |
| CHEMBL ID | 147580 |
| SCHEMBL ID | 195509 |
| MeSH ID | M0164701 |
Synonyms (26)
| Synonym |
|---|
| 80937-31-1 |
| bdbm50048201 |
| n-[6-(2,4-difluoro-phenoxy)-1-oxo-indan-5-yl]-methanesulfonamide |
| cgp-28238 |
| zk-38997 |
| flosulide |
| flosulida [inn-spanish] |
| flosulide [inn] |
| flosulidum [inn-latin] |
| 6-(2,4-difluorophenoxy)-5-methylsulfonylamino-1-indanone |
| n-(6-(2,4-difluorophenoxy)-1-oxo-5-indanyl)methanesulfonamide |
| CHEMBL147580 , |
| n-[6-(2,4-difluorophenoxy)-1-oxo-2,3-dihydroinden-5-yl]methanesulfonamide |
| flosulida |
| unii-gvr41s4zhj |
| flosulidum |
| gvr41s4zhj , |
| CXJONBHNIJFARE-UHFFFAOYSA-N |
| SCHEMBL195509 |
| DTXSID20230807 |
| HY-U00083 |
| CS-6735 |
| zk 38997;cgp 28238 |
| Q27279307 |
| n-(6-(2,4-difluorophenoxy)-1-oxo-2,3-dihydro-1h-inden-5-yl)methanesulfonamide |
| AKOS040733171 |
Research Excerpts
Actions
| Excerpt | Reference | Relevance |
|---|---|---|
| "flosulide, the increase in body weight was close to significance (0.86 vs -0.08 kg with placebo)." | ( Renal and endocrine effects of flosulide, after single and repeated administration to healthy volunteers. Brunel, P; Guyene, TT; Hornych, A; Ménard, J; Sioufi, A; Turri, M, 1995) | 1.3 |
Treatment
Treatment with flosulide reduced the proteinuria to 26.1 +/- 9 mg/24 hr at 3 mg flosumide/kg body wt/day. The treatment was equivalent to a reduction of proteinuria by a maximum of 65% (P < 0.05)
| Excerpt | Reference | Relevance |
|---|---|---|
| "Treatment with flosulide significantly reduced proteinuria as compared to aspirin treatment (64+/-15 vs." | ( Different actions of the cyclooxygenase 2 selective inhibitor flosulide in rats with passive Heymann nephritis. Grabensee, B; Heering, P; Heise, G; Schrör, K, 1998) | 0.88 |
| "Treatment with flosulide reduced the proteinuria to 26.1 +/- 9 mg/24 hr at 3 mg flosulide/kg body wt/day and 35.5 +/- 6 mg/24 hr at 9 mg/kg body wt/day, which was equivalent to a reduction of proteinuria by a maximum of 65% (P < 0.05)." | ( Effect of flosulide, a selective cyclooxygenase 2 inhibitor, on passive heymann nephritis in the rat. Bach, D; Blume, C; Gerhardz, CD; Grabensee, B; Heering, P; Heise, G; Mühlfeld, A; Schrör, K, 1999) | 1.05 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " Despite excellent bioavailability and the long plasma half-life of HN-56249, anti-inflammatory effects in rodents were only moderate." | ( Pharmacology of a selective cyclooxygenase-2 inhibitor, HN-56249: a novel compound exhibiting a marked preference for the human enzyme in intact cells. Berg, J; Blaschke, H; Christoph, T; Fellier, H; Hartmann, M; Kremminger, P; Rovensky, F; Stimmeder, D; Towart, R, 2000) | 0.31 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " Compound 20 has an efficacy profile that is superior or comparable to that of the nonselective COX inhibitor indomethacin in animal models of inflammation, pain, and fever and appears to be nonulcerogenic within the dosage ranges required for functional efficacy." | ( Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. Black, WC; Chan, CC; Ford-Hutchinson, AW; Gauthier, JY; Gordon, R; Guay, D; Kargman, S; Lau, CK; Li, CS; Mancini, J, 1995) | 0.29 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (2)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Prostaglandin G/H synthase 1 | Homo sapiens (human) | IC50 (µMol) | 50.0000 | 0.0002 | 1.5574 | 10.0000 | AID161326 |
| Prostaglandin G/H synthase 2 | Homo sapiens (human) | IC50 (µMol) | 0.0210 | 0.0001 | 0.9950 | 10.0000 | AID162338 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (60)
Molecular Functions (8)
Ceullar Components (13)
Bioassays (8)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID162338 | In vitro inhibition of prostaglandin G/H synthase 2 expressed in human osteosarcoma 143 cells | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. |
| AID177198 | In vivo antiinflammatory activity by the Carrageenan-induced rat paw edema assay. | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. |
| AID17967 | Bioavailability in squirrel monkey | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. |
| AID161326 | Inhibition of Prostaglandin G/H synthase 1 in human U937 cells | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. |
| AID23818 | Plasma terminal half life in squirrel monkeys at a dose of 1 mg/kg administered intravenously | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. |
| AID17966 | Bioavailability in rat | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. |
| AID15518 | Plasma Clearance rate was determined for the compound in squirrel monkeys | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. |
| AID15517 | Plasma Clearance rate was determined for the compound in rats | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (29)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 2 (6.90) | 18.7374 |
| 1990's | 23 (79.31) | 18.2507 |
| 2000's | 4 (13.79) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 17.11
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (17.11) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 3 (9.68%) | 5.53% |
| Reviews | 1 (3.23%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 27 (87.10%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||